Zobrazeno 1 - 10
of 43
pro vyhledávání: '"Bindi, Sohal"'
Autor:
Valerie M. Kramlinger, Christine E. Dunne, Amanda L. Cirello, Jennifer L. Dumouchel, Upendra A. Argikar, Bindi Sohal, Mithat Gunduz
Publikováno v:
Journal of Pharmaceutical Sciences. 106:2276-2281
The liver is known to be the principal site of drug metabolism. Depending on the route of administration, especially in cases of topical and local delivery, evaluation of local drug metabolism in extrahepatic tissues is vital to assess fraction of th
Autor:
Richard Aspinall, Mustafa Shennak, George Stocia, Dean Quinn, Lali Javashvili, Valentina Molteni, Chinweike Ukomadu, Bindi Sohal, Yiming Zhang, Miljen Martic, Alexandre Avrameas, Sheena Kao, Jacques Herve, Rachel Soon, Michael Badman
Publikováno v:
Journal of Hepatology. 73:S4-S5
Autor:
Catherine Ritchie, Lucy Barker, Matthew Bm Thomas, Jodie Manini, Elisabeth Willard, Jennifer Willis, Zarin Brown, Edward Charles Hall, Gareth Williams, Ryan West, Steven J. Charlton, David Andrew Sandham, Lyndon Nigel Brown, Simon J. Watson, Janet Maas, Devnandan Chatterjee, David A. Sykes, Nicholas Duggan, Katharine L. Turner, Gerald Dubois, David C. Budd, Bindi Sohal, Rowan Stringer, Rachael Profit, Darren Riddy, Duncan Shaw, Julia Hatto, Brian Cox
Further optimization of an initial DP2 receptor antagonist clinical candidate NVP-QAV680 led to the discovery of a follow-up molecule 2-(2-methyl-1-(4-(methylsulfonyl)-2-(trifluoromethyl)benzyl)-1H-pyrrolo[2,3-b]pyridin-3-yl)acetic acid (compound 11,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e65a3f67567222f76078480d2373e99e
https://europepmc.org/articles/PMC5430394/
https://europepmc.org/articles/PMC5430394/
Autor:
Gareth Williams, Rowan Stringer, Eckhard Weber, Jonathan Rose, Andrew James Culshaw, Bindi Sohal, Jeffrey Mckenna
Publikováno v:
Xenobiotica. 44:902-912
1. The pharmacokinetic properties and metabolism of NVS-CRF38 [7-(3,5-dimethyl-1H-1,2,4-triazol-1-yl)-3-(4-methoxy-2-methylphenyl)-2,6-dimethylpyrazolo[5,1-b]oxazole], a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist, were determin
Autor:
Bindi Sohal, Gareth Williams, Olivier Kretz, Joel Krauser, Franck Picard, Rowan Stringer, Jeffrey Mckenna
Publikováno v:
Drug Metabolism and Disposition. 42:954-962
Deuterium isotope effects were evaluated as a strategy to optimize the pharmacokinetics of 7-(3,5-dimethyl-1H-1,2,4-triazol-1-yl)-3-(4-methoxy-2-methylphenyl)-2,6-dimethylpyrazolo[5,1-b]oxazole (NVS-CRF38), a novel corticotropin-releasing factor rece
Autor:
Brian Cox, David C. Budd, Anna King, Gareth Williams, Nicholas Duggan, Rowan Stringer, Marcus Furegati, Alfred Schmidt, Josef G. Meingassner, Kamlesh Bala, Brian Everatt, Katharine L. Turner, Jennifer Simmons, Cerys Docx, Catherine Leblanc, Gerald Dubois, Frank Kalthoff, Caroline Wilson, Lucy Barker, Karen England, Nicola Arnold, John Westwick, Edward Charles Hall, Bindi Sohal, Jennifer Willis, Heinrich Aschauer, David Andrew Sandham, Rachael Profit, Zarin Brown, Lyndon Nigel Brown, Simon J. Watson, Jodie Manini, Christoph Walker, Matthew Thomas
Publikováno v:
Bioorganic & Medicinal Chemistry. 21:6582-6591
Optimization of a 7-azaindole-3-acetic acid CRTh2 receptor antagonist chemotype derived from high throughput screening furnished a highly selective compound NVP-QAV680 with low nM functional potency for inhibition of CRTh2 driven human eosinophil and
Autor:
Sandra Sanabria, Laura Vessy, H. Donald Burns, Jean-Claude Baron, Richard Hargreaves, Michael L. Schrag, José M. Vega, Robert F. Dannals, Raymond E. Gibson, John S. Beech, Dean F. Wong, John R. Atack, Wai Si Eng, Ruth M. McKernan, Franklin I. Aigbirhio, Tim D. Fryer, Paul Scott-Stevens, Bindi Sohal, Christine Ryan, Yun Zhou
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 332:17-25
The GABA(A) receptor alpha2/alpha3 subtype-selective compound 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023; also known as MK-0777) is a triazolopyridazine that has similar,
Autor:
Ray E Gibson, Gerard R. Dawson, Wai-Si Eng, H. Donald Burns, Barbara Francis, Christine Ryan, Bindi Sohal, John R. Atack, Richard Hargreaves
Publikováno v:
British Journal of Pharmacology. 157:796-803
alpha5IA (3-(5-methylisoxazol-3-yl)-6-[(1-methyl-1,2,3-triazol-4-yl)methyloxy]-1,2,4-triazolo[3,4-a]phthalazine) is a triazolophthalazine with subnanomolar affinity for alpha1-, alpha2-, alpha3- and alpha5-containing GABA(A) receptors. Here we have e
Publikováno v:
Journal of Pharmaceutical Sciences. 97:4586-4595
Equilibrium dialysis (ED) is one of the most frequently used approaches to investigate drug binding, where the major drawbacks are the time to reach equilibrium (varying between 6 and 24 h), a long assay preparation time and complexity of automation.
Autor:
Andrew Madin, Tim Sparey, Timothy Harrison, Joanne Clare Hannam, Mark S. Shearman, Earl E. Clarke, Bindi Sohal
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:375-379
Bridgehead substituted derivatives of bicyclo[4.2.1]nonanes were synthesized and shown to be potent inhibitors of gamma-secretase. Two related series were synthesized to explore the SARs. More potent compounds were found in the non-benzofused series